Furoxans (Oxadiazole-4N-oxides) with Attenuated Reactivity are Neuroprotective, Cross the Blood Brain Barrier, and Improve Passive Avoidance Memory

Journal of Medicinal Chemistry
2018.0

Abstract

Nitric oxide (NO) mimetics and other agents capable of enhancing NO/cGMP signaling have demonstrated efficacy as potential therapies for Alzheimer's disease. A group of thiol-dependent NO mimetics known as furoxans may be designed to exhibit attenuated reactivity to provide slow onset NO effects. The present study describes the design, synthesis, and evaluation of a furoxan library resulting in the identification of a prototype furoxan, 5a, which was profiled for use in the central nervous system. Furoxan 5a demonstrated negligible reactivity toward generic cellular thiols under physiological conditions. Nonetheless, cGMP-dependent neuroprotection was observed, and 5a (20 mg/kg) reversed cholinergic memory deficits in a mouse model of passive avoidance fear memory. Importantly, 5a can be prepared as a pharmaceutically acceptable salt and is observed in the brain 12 h after oral administration, suggesting potential for daily dosing and excellent metabolic stability. Continued investigation into furoxans as attenuated NO mimetics for the CNS is warranted.

Knowledge Graph

Similar Paper

Furoxans (Oxadiazole-4N-oxides) with Attenuated Reactivity are Neuroprotective, Cross the Blood Brain Barrier, and Improve Passive Avoidance Memory
Journal of Medicinal Chemistry 2018.0
Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents
European Journal of Medicinal Chemistry 2014.0
Imidazolylacetophenone oxime-based multifunctional neuroprotective agents: Discovery and structure-activity relationships
European Journal of Medicinal Chemistry 2022.0
Identification of Highly Promising Antioxidants/Neuroprotectants Based on Nucleoside 5′-Phosphorothioate Scaffold. Synthesis, Activity, and Mechanisms of Action
Journal of Medicinal Chemistry 2015.0
Design, synthesis, and biological evaluation of novel (4-(1,2,4-oxadiazol-5-yl)phenyl)-2-aminoacetamide derivatives as multifunctional agents for the treatment of Alzheimer's disease
European Journal of Medicinal Chemistry 2022.0
Design and Synthesis of Neuroprotective Methylthiazoles and Modification as NO-Chimeras for Neurodegenerative Therapy
Journal of Medicinal Chemistry 2012.0
Design, synthesis and biological evaluation of pyranocarbazole derivatives against Alzheimer’s disease, with antioxidant, neuroprotective and cognition enhancing properties
Bioorganic Chemistry 2022.0
(3R,5S,7as)-(3,5-Bis(4-fluorophenyl)tetrahydro-1H-oxazolo[3,4-c]oxazol-7a-yl)methanol, a Novel Neuroprotective Agent
Journal of Medicinal Chemistry 2009.0
Old phenothiazine and dibenzothiadiazepine derivatives for tomorrow’s neuroprotective therapies against neurodegenerative diseases
European Journal of Medicinal Chemistry 2010.0
Novel cinnamamide-dibenzylamine hybrids: Potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease
European Journal of Medicinal Chemistry 2017.0